Autophosphorylation of kinases influences their conformational state and can also regulate enzymatic activity. Recently, this has become an area of interest for drug discovery. Using Alk2 as an example, we present two protocols - one based on phosphate-binding Alphascreen beads, the other on coupled luminescence measurements of ADP formation - that can be used to screen for inhibitors of autophosphorylation.
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http://dx.doi.org/10.1007/978-1-4939-3673-1_10 | DOI Listing |
PLoS One
January 2025
Special Infectious Agents Unit-BSL3, King Fahd Medical Research Center, King Abdulaziz University, Jeddah, Saudi Arabia.
The ongoing increase in the prevalence and mutation rate of the influenza virus remains a critical global health issue. A promising strategy for antiviral drug development involves targeting the RNA-dependent RNA polymerase, specifically the PB2-cap binding domain of Influenza A H5N1. This study employs an in-silico approach to inhibit this domain, crucial for viral replication, using potential inhibitors derived from marine bacterial compounds.
View Article and Find Full Text PDFAdv Sci (Weinh)
January 2025
Department of Surgery, Center for Cancer Medicine, the Fourth Affiliated Hospital of School of Medicine, International School of Medicine, International Institutes of Medicine, Zhejiang University, Yiwu, 322000, China.
Irreversible electroporation (IRE) is a novel local tumor ablation technique that can potentially stimulate immune responses. However, IRE alone cannot effectively activate the immune system or prevent distant metastases. Therefore, this study utilized the biocompatibility of Chlorella vulgaris (C.
View Article and Find Full Text PDFAsian Pac J Cancer Prev
January 2025
Department of Biotechnology, Kakatiya University, Warangal, Telangana, India.
Objective: A new library of Thiazolidine-2,4-dione-biphenyl Derivatives derivatives (10a-j) was designed and synthesized. All compounds were characterized by spectral data. Further, these were evaluated for their in vitro anticancer activity.
View Article and Find Full Text PDFClin Transl Oncol
January 2025
Medical Oncology Department, Faculty of Medicine, School of Medicine, Cebeci Hospital, Ankara University, Dikimevi, 06590, Ankara, Turkey.
Purpose: Immunotherapy efficacy in elderly patients with comorbidities and poor performance status is not well understood. More knowledge on this topic is needed to identify subgroups that will benefit from immunotherapy. We aimed to evaluate the effect of comorbidity burden in patients receiving immunotherapy.
View Article and Find Full Text PDFArch Dermatol Res
January 2025
Department of Nursing, University of Peloponnese, Tripoli, 22100, Greece.
Multiple parameters define the treatment course with biologics for a psoriatic patient while treatment switches are often associated with worse prognosis. The purpose of this study was to describe the switching patterns of biologics for psoriasis in the Greek market landscape and to detect associated factors that may impact the evolvement of selected therapy. This is a retrospective cohort study using data recorded in the nationwide digital prescription database of Greece.
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